Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of Glucocorticoid Receptor (GR) translocation. Furthermore, the subject compounds and compositions are useful for the treatment of diseases involved in the hypothalamic-pituitary-adrenal (HPA) axis.

Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.

Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

Abstract: An N-substituted polyamideimide essentially composed of identical or different repeating units of the formula I ##STR1## where R.sup.1 is one of the following tetravalent aromatic radicals ##STR2## and X is a bond or one of the following linkers ##STR3## where R.sup.2 and R.sup.4 are each, independently of one another, one of the following divalent aromatic radicals ##STR4## and where X has the abovementioned meanings and where R.sup.3 is hydrogen or a monovalent radical such as C.sub.1 -C.sub.6 -alkyl or phenyl, and the C.sub.1 -C.sub.6 -alkyl-, C.sub.1 -C.sub.6 -alkoxy-, aryl- or halogen-substituted derivatives thereof, and precursors (monomers) therefor, are described.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.

Abstract: Compounds of the formula ##STR1## wherein: z is O or I;X is ##STR2## a and b are 0, 1, or 2 and a+b=0, 1 or 2; R, R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, alkyl or aralkyl;R.sub.n is hydrogen, alkyl, aralkyl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl or amidino;R.sup.5 groups on vicinal carbon atoms may together form a carbon-carbon double bond when a or b=2;R groups on vicinal carbon atoms may together form a carbon-carbon double bond when R.sub.n is hydrogen and z=1;R.sup.4 and R.sup.5 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;R.sup.5 and R.sup.6 groups may together form a carbon-nitrogen double bond when R.sub.3 is hydrogen and a+b=1;R.sup.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;Y is hydrogen, --O--R.alpha., --S-R.alpha. or ##STR3## R.alpha. is hydrogen, alkyl, cycloalkyl or acyl; R.beta. is hydrogen or alkyl; andR.alpha. and R.beta.

Abstract: A compound for treating disorders of the central nervous system, which is of the formulawherein A taken together with the two carbon atoms denoted by .alpha. and .beta. is one of the following groups: ##STR1## R.sup.1 is one of the following groups:--CH.dbd.CH--R.sup.6 (d)and--C.tbd.C--R.sup.6, (e)R.sup.2 is hydrogen, R.sup.3 is lower alkyl, or R.sup.2 and R.sup.3 together are dimethylene or trimethylene, R.sup.4 and R.sup.5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R.sup.6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C.sub.3 -C.sub.7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R.sup.6 is different from hydrogen.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract: Metal values are extracted from aqueous solutions containing halide or pseudohalide anion using 1,1'-substituted 2,2'-biimidazole or bibenzimidazole compounds. Useful for the solvent extraction of zinc and copper from chloride leach solutions.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinonepryidazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.

Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.